الفهرس 
Title : Synthesis and biological activity evaluation of some unsaturated carbonyl derivatives
ContantsOnly 14 pages are availabe for public view
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Abstract
In the light of the advancement, uniqueness, and potential extensive use of medication design and therapy, a new series of bis(cyanoacrylamides) of various carbon-chain lengths incorporating sulphamethoxazole derivatives (7a-7f) were prepared and confirmed by different spectral analysis tools. The in vitro cytotoxic activities of the synthesized compounds against a group of human cancer cell lines (HCT116, MDA-MB-231 and A549) were evaluated. Among them, 4C- and 6C-spacer derivatives (7e and 7f) showed the most promising anti-proliferative activities against the HCT116 cell lines with IC50 values of 39.7 ± 0.8 and 28.5 ± 0.5 μM, respectively. The results revealed that these compounds have low toxicity. Investigation of the apoptotic activity of the most active compounds revealed that compounds 7e and 7f could induce apoptosis of HCT116. These compounds also induced a significant increase in the caspase-3 activities, remarkable downregulation of the Bcl-2, and significant upregulation of the CDH1 by using ELISA. DNA cleavage activities were determined using gel electrophoresis. Furthermore, 7e and 7f also proved to have a good DNA binding affinity using UV-Vis and EB-displacements measurements. Moreover, a molecular docking study for 7e and 7f was performed to predict their binding affinities toward the active site of different protein sets (Bcl2, CDH1 and BSA). Results of molecular docking were strongly correlated with that of the cytotoxicity study.